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Covalent Activators Of K2p Channels
University of California, San Francisco
Small molecule
Cardiovascular disease
Hit To Lead or Lead Optimization
The newly identified chemical probes consist of an aromatic region that specifically binds to a novel allosteric pocket unique to the TREK1 potassium ion channel, as well as an electrophilic moiety that binds to the channel. Treating cells expressing wild-type K2P or mutant channels with the appropriate electrophile results in 2-5-fold activation of the channel over baseline activity.
US 9862684 B2